CAJ | 학술논문

为了寻找开发高效低毒的1，3，4-二唑类抗菌物质，超声辅助条件下以四丁基氢氧化磷为相转移催化剂，高选择性制得2-烯丙基硫代水杨酸和2-苄基硫代水杨酸（2a、2b）。以上述硫代水杨酸和芳香肼为原料，硅胶负载丙基磷酸环酐为催化剂，在三乙胺存在下，设置微波功率为800 W，辐射时间为8 min 或10 min，通过缩合反应合成了2-（2-硫醚苯基）-5-芳基-1，3，4-二唑类似化合物（4a～4f），目标化合物的合成收率为81％～88％，其结构经 IR、1 HNMR 和元素分析等测试技术得以证实。初步抗菌试验结果表明所制备的2-（2-硫醚苯基）-5-芳基-1，3，4-二唑对枯草杆菌的抗菌活性较为显著，除4d 和4f 外对大肠杆菌和金黄色葡萄球菌有一定程度的抑制作用。
위료심조개발고효저독적1，3，4-이서류항균물질，초성보조조건하이사정기경양화린위상전이최화제，고선택성제득2-희병기류대수양산화2-변기류대수양산（2a、2b）。이상술류대수양산화방향정위원료，규효부재병기린산배항위최화제，재삼을알존재하，설치미파공솔위800 W，복사시간위8 min 혹10 min，통과축합반응합성료2-（2-류미분기）-5-방기-1，3，4-이서유사화합물（4a～4f），목표화합물적합성수솔위81％～88％，기결구경 IR、1 HNMR 화원소분석등측시기술득이증실。초보항균시험결과표명소제비적2-（2-류미분기）-5-방기-1，3，4-이서대고초간균적항균활성교위현저，제4d 화4f 외대대장간균화금황색포도구균유일정정도적억제작용。
In order to develop new l,3,4-oxadiazoles with high activity and low toxicity,an efficient etherification of thiosalicylic acid via the allyl or benzyl halides in presence of tetrabutylphosphonium hydroxide as a phase transfer catalyst under ultrasound ir-radiation was studied,which was used to further react with aryl carboxylic acid hydrazides in the presence of silica gel supported propylphosphonic anhydride as the dehydration reagent at the base condition of Et3 N under microwave irradiation at the power of 800 W in 8-10 minutes for the synthesis of 2-(2-sulfanyl-phenyl)-5-aryl-l,3,4-oxadiazoles(4a-4f)with a yield of 81%-88%,re-spectively.The structures of the corresponding products were characterized by the means of IR,1 HNMR spectra and elemental analysis.The preliminary bioassay results show that the titled compounds have strong antibacterial activities against Bacillus Subtilis ,and have certain different effects of antibacterial against Escherichia Coli ,Staphylococcus Aureus except for the two l, 3,4-oxadiazoles 4d and 4f.